EP3554506A4 - Bycyclic heteroaryl derivatives as cftr potentiators - Google Patents

Bycyclic heteroaryl derivatives as cftr potentiators Download PDF

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Publication number
EP3554506A4
EP3554506A4 EP17879832.8A EP17879832A EP3554506A4 EP 3554506 A4 EP3554506 A4 EP 3554506A4 EP 17879832 A EP17879832 A EP 17879832A EP 3554506 A4 EP3554506 A4 EP 3554506A4
Authority
EP
European Patent Office
Prior art keywords
heteroaryl derivatives
cftr potentiators
bycyclic
bycyclic heteroaryl
potentiators
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP17879832.8A
Other languages
German (de)
French (fr)
Other versions
EP3554506A1 (en
EP3554506B1 (en
Inventor
Joseph Walter Strohbach
David Christopher Limburg
John Paul Mathias
Atli Thorarensen
James John MOUSSEAU
Rajiah Aldrin DENNY
Christoph Wolfgang Zapf
Ivan Viktorovich Efremov
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cystic Fibrosis Foundation
Original Assignee
Cystic Fibrosis Foundation
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Publication date
Application filed by Cystic Fibrosis Foundation filed Critical Cystic Fibrosis Foundation
Publication of EP3554506A1 publication Critical patent/EP3554506A1/en
Publication of EP3554506A4 publication Critical patent/EP3554506A4/en
Application granted granted Critical
Publication of EP3554506B1 publication Critical patent/EP3554506B1/en
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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EP17879832.8A 2016-12-16 2017-12-14 Bycyclic heteroaryl derivatives as cftr potentiators Active EP3554506B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662435253P 2016-12-16 2016-12-16
PCT/US2017/066317 WO2018112149A1 (en) 2016-12-16 2017-12-14 Bycyclic heteroaryl derivatives as cftr potentiators

Publications (3)

Publication Number Publication Date
EP3554506A1 EP3554506A1 (en) 2019-10-23
EP3554506A4 true EP3554506A4 (en) 2020-06-10
EP3554506B1 EP3554506B1 (en) 2021-04-28

Family

ID=62557188

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17879832.8A Active EP3554506B1 (en) 2016-12-16 2017-12-14 Bycyclic heteroaryl derivatives as cftr potentiators

Country Status (11)

Country Link
US (4) US10131670B2 (en)
EP (1) EP3554506B1 (en)
JP (1) JP7150721B2 (en)
CN (1) CN110300589B (en)
AU (2) AU2017378324B2 (en)
BR (1) BR112019012335A2 (en)
CA (1) CA3046968A1 (en)
MX (1) MX2019007135A (en)
RU (1) RU2753056C2 (en)
SG (2) SG10201911221RA (en)
WO (1) WO2018112149A1 (en)

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TWI735416B (en) 2014-10-06 2021-08-11 美商維泰克斯製藥公司 Modulators of cystic fibrosis transmembrane conductance regulator
KR20180082556A (en) 2015-11-25 2018-07-18 길리어드 아폴로, 엘엘씨 Pyrazole ACC inhibitors and uses thereof
SI3379933T1 (en) 2015-11-25 2023-07-31 Gilead Apollo, Llc Fungicidal compositions containing derivatives of 2,4-dioxo-1,4-dihydrothieno(2,3-d)pyrimidine
HUE053175T2 (en) 2015-11-25 2021-06-28 Gilead Apollo Llc Ester acc inhibitors and uses thereof
KR20180082557A (en) 2015-11-25 2018-07-18 길리어드 아폴로, 엘엘씨 Triazole ACC inhibitors and uses thereof
CN109803962B (en) 2016-09-30 2022-04-29 弗特克斯药品有限公司 Modulators of cystic fibrosis transmembrane conductance regulator proteins, and pharmaceutical compositions
MA54847A (en) 2016-12-09 2021-12-08 Vertex Pharma CRYSTALLINE FORM OF AN N-(PYRAZOL-4-YL)SULFONYL-6-(PYRAZOL-1-YL)-2-(PYRROLIDIN-1-YL)PYRIDINE-3-CARBOXAMIDE FOR TREATING VUD
EP3634402A1 (en) 2017-06-08 2020-04-15 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2019018395A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
ES2912657T3 (en) 2017-08-02 2022-05-26 Vertex Pharma Processes for preparing pyrrolidine compounds
AU2018351533B2 (en) 2017-10-19 2023-02-02 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of CFTR modulators
KR20200097293A (en) 2017-12-08 2020-08-18 버텍스 파마슈티칼스 인코포레이티드 Method for producing a modulator of cystic fibrosis transmembrane conduction modulator
TWI810243B (en) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 Pharmaceutical compositions for treating cystic fibrosis
CN112004817B (en) 2018-02-15 2023-06-23 弗特克斯药品有限公司 Macrocyclic compounds as modulators of CFTR, pharmaceutical compositions thereof, their use and methods of preparation
US11414439B2 (en) 2018-04-13 2022-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
AR118555A1 (en) * 2019-04-03 2021-10-20 Vertex Pharma MODULATING AGENTS OF THE TRANSMEMBRANE CONDUCTANCE REGULATOR OF CYSTIC FIBROSIS
KR20220019015A (en) * 2019-06-10 2022-02-15 노파르티스 아게 Pyridine and pyrazine derivatives for the treatment of CF, COPD, and bronchiectasis
JP2022541178A (en) 2019-07-15 2022-09-22 ノバルティス アーゲー (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide preparations
CN114599657A (en) 2019-08-14 2022-06-07 弗特克斯药品有限公司 Crystalline forms of a CFTR modulator
TW202120517A (en) 2019-08-14 2021-06-01 美商維泰克斯製藥公司 Process of making cftr modulators
TW202115092A (en) 2019-08-14 2021-04-16 美商維泰克斯製藥公司 Modulators of cystic fibrosis transmembrane conductance regulator
CA3188234A1 (en) 2020-08-20 2022-02-24 Jeffrey Axelrod Methods for treating respiratory diseases characterized by mucus hypersecretion
CN112876524B (en) * 2021-01-26 2022-10-28 上海法默生物科技有限公司 Preparation method of Reideciclovir intermediate

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WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
WO2007079164A2 (en) * 2005-12-29 2007-07-12 Abbott Laboratories Protein kinase inhibitors
EP3541390A1 (en) * 2016-11-18 2019-09-25 Cystic Fibrosis Foundation Therapeutics Inc. Pyrrolopyrimidines as cftr potentiators

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DE10135815A1 (en) 2001-07-23 2003-02-06 Bayer Ag Use of imidazo-triazinone derivative phosphodiesterase 5 inhibitors e.g. for treatment of cardiac insufficiency, psoriasis, diabetes, cancer, glaucoma, bladder disease, Parkinson's disease or pain
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7429596B2 (en) * 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
JP5249776B2 (en) 2005-12-02 2013-07-31 バイエル・ヘルスケア・エルエルシー Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyperproliferative diseases and diseases associated with angiogenesis
PT2004654E (en) * 2006-04-04 2013-08-27 Univ California Pyrazolopyrimidine derivatives for use as kinase antagonists
BRPI0820342A2 (en) * 2007-11-07 2015-05-26 Foldrx Pharmaceuticals Inc Protein Traffic Modulation
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UY34484A (en) * 2011-12-15 2013-07-31 Bayer Ip Gmbh BENZOTIENILO-PIRROLOTRIAZINAS DISUSTITUIDAS AND ITS USES
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Patent Citations (3)

* Cited by examiner, † Cited by third party
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WO2004100868A2 (en) * 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
WO2007079164A2 (en) * 2005-12-29 2007-07-12 Abbott Laboratories Protein kinase inhibitors
EP3541390A1 (en) * 2016-11-18 2019-09-25 Cystic Fibrosis Foundation Therapeutics Inc. Pyrrolopyrimidines as cftr potentiators

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
S. M. ROWE ET AL: "Cystic Fibrosis Transmembrane Regulator Correctors and Potentiators", COLD SPRING HARBOR PERSPECTIVES IN MEDICINE, vol. 3, no. 7, 1 July 2013 (2013-07-01), pages a009761 - a009761, XP055559276, DOI: 10.1101/cshperspect.a009761 *
See also references of WO2018112149A1 *

Also Published As

Publication number Publication date
EP3554506A1 (en) 2019-10-23
WO2018112149A1 (en) 2018-06-21
SG10201911221RA (en) 2020-02-27
US20190016727A1 (en) 2019-01-17
US10377762B2 (en) 2019-08-13
CN110300589A (en) 2019-10-01
CA3046968A1 (en) 2018-06-21
RU2019120990A3 (en) 2021-01-18
US10131670B2 (en) 2018-11-20
BR112019012335A2 (en) 2020-03-03
MX2019007135A (en) 2019-11-18
AU2017378324A1 (en) 2019-06-27
US20180170938A1 (en) 2018-06-21
SG10201911076QA (en) 2020-01-30
US10208053B2 (en) 2019-02-19
EP3554506B1 (en) 2021-04-28
CN110300589B (en) 2023-03-10
JP2020502103A (en) 2020-01-23
AU2017378324B2 (en) 2021-09-02
US20190016728A1 (en) 2019-01-17
RU2019120990A (en) 2021-01-18
JP7150721B2 (en) 2022-10-11
RU2753056C2 (en) 2021-08-11
AU2021277702B2 (en) 2023-11-30
US20190330219A1 (en) 2019-10-31
US10766904B2 (en) 2020-09-08
AU2021277702A1 (en) 2021-12-23

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